Even though several quinazolinone derivatives have been synthesized, still there is a constant demand for designing and synthesis of new quinazolinone derivatives by fine‐tuning the electronic and steric properties of substituents due to their interesting structure‐based biological utilities and the versatile chemistry. While many of the synthetic routes are useful as building blocks in synthetic organic chemistry, the drawbacks of some of these methods like unsatisfactory or variable yields, prolonged reaction times, inadequate tolerance to other substrates, including the use of costly catalysts/reagents. This review article is mainly focused on various synthetic routes for the preparation of quinazolinones, their important properties and applications.

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A highly efficient, three-component one-pot and L-proline catalyzed Knoevenagel condensation reaction of substituted-2phenoxyquinoline-3-carbaldehyde, 1,3-cyclohexanedione/dimedone or ammonium acetate is described. These reactions afford unexpected products of xanthene and acridine based quinolones in ethanol with good yields. All these isolated products are characterised by spectroscopic and analytical data.[a] M.

A new synthetic route for the preparation of aromatic 1,5‐diketones was developed through Ni(II)‐diphosphine‐catalyzed one‐pot reactions of various aromatic ketones with aromatic aldehydes in presence of KOH and 1,4‐dioxane in moderate yields. This protocol provides expeditious access to aromatic 1,5‐diones with a single step through cross‐aldol reaction followed by Michael 1,4‐addition and does not require expensive metal complexes as catalysts. All the synthesized catalysts and the products derived from the carbonyl compounds were fully characterized by spectroscopic and analytical data. The factors influencing the rate of reaction were discussed.

The inhibition of phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit alpha (PIK3CA) protein could be a promising treatment for breast cancer. In this regard, docking studies were accomplished on various functionalized organic molecules. Among them, several derivatives of quinazolin-4(1H)-one exhibited anti-breast cancer activity and satisfied the drug likeliness properties. Further, the in vitro inhibitory studies by a series of 2-(2-phenoxyquinolin-3-yl)-2,3-dihydroquinazolin-4(1H)-one molecules showed strong anti-cancer activity than the currently available drug, wortmannin. The MTT cytotoxicity assay was used to predict the anti-proliferative activity of these drugs against MCF-7 cancer cells by inhibiting the PIK3CA protein. The dose-dependent analysis showed a striking decrease in cancer cell viability at 24 h with inhibitory concentrations (IC 50 ) of 3b, 3c, 3d, 3f and 3m are 15 � 1, 17 � 1, 8 � 1, 10 � 1 and 60 � 1 (nanomoles), respectively. This is the first report in the literature on the inhibition of PIK3CA protein by quinazolinone derivatives that can be used in the treatment of cancer. Quinazolinone analogs have the potential to be safe and economically feasible scaffolds if they are produced using a chemical technique that is both straightforward and amenable to modification. From the cancer research perspective, this study can eventually offer better care for cancer patients.